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WO2010075983A8 - Procédé pour la production de bivalirudine - Google Patents

Procédé pour la production de bivalirudine Download PDF

Info

Publication number
WO2010075983A8
WO2010075983A8 PCT/EP2009/009080 EP2009009080W WO2010075983A8 WO 2010075983 A8 WO2010075983 A8 WO 2010075983A8 EP 2009009080 W EP2009009080 W EP 2009009080W WO 2010075983 A8 WO2010075983 A8 WO 2010075983A8
Authority
WO
WIPO (PCT)
Prior art keywords
gly
glu
pro
bivalirudin
production
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2009/009080
Other languages
English (en)
Other versions
WO2010075983A1 (fr
Inventor
Geoffroy Sommen
Luciano Forni
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Lonza Braine SA
Lonza AG
Original Assignee
Lonza Braine SA
Lonza AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to CA2744627A priority Critical patent/CA2744627C/fr
Priority to MX2011006950A priority patent/MX2011006950A/es
Priority to DK09795927.4T priority patent/DK2382232T3/da
Priority to HK12102674.5A priority patent/HK1162527B/xx
Priority to JP2011543985A priority patent/JP5730781B2/ja
Priority to SG2011039179A priority patent/SG171859A1/en
Priority to ES09795927.4T priority patent/ES2439502T3/es
Priority to CN200980152943.3A priority patent/CN102264757B/zh
Priority to US13/139,956 priority patent/US8921517B2/en
Priority to AU2009335350A priority patent/AU2009335350A1/en
Priority to EA201101015A priority patent/EA201101015A1/ru
Priority to BRPI0923848A priority patent/BRPI0923848A2/pt
Application filed by Lonza Braine SA, Lonza AG filed Critical Lonza Braine SA
Priority to EP09795927.4A priority patent/EP2382232B1/fr
Publication of WO2010075983A1 publication Critical patent/WO2010075983A1/fr
Publication of WO2010075983A8 publication Critical patent/WO2010075983A8/fr
Priority to ZA2011/04195A priority patent/ZA201104195B/en
Priority to IL213457A priority patent/IL213457A/en
Anticipated expiration legal-status Critical
Priority to US14/552,807 priority patent/US20150080550A1/en
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81—Protease inhibitors
    • C07K14/815—Protease inhibitors from leeches, e.g. hirudin, eglin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Analytical Chemistry (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

La présente invention concerne un procédé pour la production de bivalirudine, un peptide 20-mère de formule H-D-Phe1-Pro-Arg-Pro-Gly5-Gly-Gly-Gly-Asn-Gly10-Asp-Phe-Glu-Glu-lle15-Pro-Glu-Glu-Tyr-Leu20-OH (I) via une synthèse convergente à cinq fragments, et plusieurs intermédiaires peptidiques de celle-ci.
PCT/EP2009/009080 2008-12-29 2009-12-17 Procédé pour la production de bivalirudine Ceased WO2010075983A1 (fr)

Priority Applications (16)

Application Number Priority Date Filing Date Title
EA201101015A EA201101015A1 (ru) 2008-12-29 2009-12-17 Способ получения бивалирудина
DK09795927.4T DK2382232T3 (da) 2008-12-29 2009-12-17 Fremgangsmåde til fremstilling af bivalirudin
HK12102674.5A HK1162527B (en) 2008-12-29 2009-12-17 Process for the production of bivalirudin
JP2011543985A JP5730781B2 (ja) 2008-12-29 2009-12-17 ビバリルジンの製造方法
SG2011039179A SG171859A1 (en) 2008-12-29 2009-12-17 Process for the production of bivalirudin
ES09795927.4T ES2439502T3 (es) 2008-12-29 2009-12-17 Proceso para la producción de bivalirudina
CN200980152943.3A CN102264757B (zh) 2008-12-29 2009-12-17 制备比伐卢定的方法
US13/139,956 US8921517B2 (en) 2008-12-29 2009-12-17 Process for the production of bivalirudin
AU2009335350A AU2009335350A1 (en) 2008-12-29 2009-12-17 Process for the production of bivalirudin
CA2744627A CA2744627C (fr) 2008-12-29 2009-12-17 Procede pour la production de bivalirudine
MX2011006950A MX2011006950A (es) 2008-12-29 2009-12-17 Proceso para la produccion de bivalirudina.
BRPI0923848A BRPI0923848A2 (pt) 2008-12-29 2009-12-17 processo para a produção de bivalirudina.
EP09795927.4A EP2382232B1 (fr) 2008-12-29 2009-12-17 Procédé pour la préparation de la bivalirudine
ZA2011/04195A ZA201104195B (en) 2008-12-29 2011-06-06 Process for the production of bivalirudin
IL213457A IL213457A (en) 2008-12-29 2011-06-09 Bibalirudin preparation process
US14/552,807 US20150080550A1 (en) 2008-12-29 2014-11-25 Process for the Production of Bivalirudin

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP08022479 2008-12-29
EP08022479.3 2008-12-29
US26047109P 2009-11-12 2009-11-12
US61/260,471 2009-11-12

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/139,956 A-371-Of-International US8921517B2 (en) 2008-12-29 2009-12-17 Process for the production of bivalirudin
US14/552,807 Division US20150080550A1 (en) 2008-12-29 2014-11-25 Process for the Production of Bivalirudin

Publications (2)

Publication Number Publication Date
WO2010075983A1 WO2010075983A1 (fr) 2010-07-08
WO2010075983A8 true WO2010075983A8 (fr) 2010-08-26

Family

ID=42060981

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2009/009080 Ceased WO2010075983A1 (fr) 2008-12-29 2009-12-17 Procédé pour la production de bivalirudine

Country Status (18)

Country Link
US (2) US8921517B2 (fr)
EP (1) EP2382232B1 (fr)
JP (2) JP5730781B2 (fr)
KR (1) KR101653950B1 (fr)
CN (3) CN103864894B (fr)
AR (1) AR074944A1 (fr)
AU (1) AU2009335350A1 (fr)
CA (2) CA2916716C (fr)
CO (1) CO6400148A2 (fr)
DK (1) DK2382232T3 (fr)
EA (1) EA201101015A1 (fr)
ES (1) ES2439502T3 (fr)
IL (1) IL213457A (fr)
MX (1) MX2011006950A (fr)
SG (1) SG171859A1 (fr)
TW (3) TWI599580B (fr)
WO (1) WO2010075983A1 (fr)
ZA (1) ZA201104195B (fr)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4903709B2 (ja) 2004-10-19 2012-03-28 ロンザ アーゲー 固相ペプチド合成のための方法
KR101634830B1 (ko) * 2008-09-03 2016-06-29 시노팜 타이완 리미티드 비발리루딘의 제조방법
US7985733B1 (en) 2010-01-06 2011-07-26 The Medicines Company Buffer-based method for preparing bivalirudin drug product
CN102816208B (zh) * 2011-06-10 2016-11-23 江苏豪森药业集团有限公司 一种比伐卢定的液相合成方法
CN102532274B (zh) * 2012-02-13 2014-04-23 成都圣诺生物制药有限公司 一种比伐卢定的制备方法
CN102731624B (zh) * 2012-06-14 2015-09-23 无锡市凯利药业有限公司 一种固相片段法合成比伐卢定的方法
CN102702325B (zh) * 2012-06-19 2015-09-23 深圳翰宇药业股份有限公司 一种抗凝血多肽的制备方法
WO2013192430A2 (fr) * 2012-06-20 2013-12-27 The Regents Of The University Of California Catalyseur biomimétique dynamique de type synzyme, catalyse, et systèmes catalytiques
WO2014032257A1 (fr) * 2012-08-30 2014-03-06 深圳翰宇药业股份有限公司 Procédé de préparation de bivalirudine
CN103965293B (zh) * 2013-02-05 2020-02-14 深圳信立泰药业股份有限公司 一种高纯度比伐卢定及其工业化制备方法
CN103242431B (zh) * 2013-05-20 2015-05-13 齐鲁制药有限公司 一种比伐卢定的制备方法
CN110204611B (zh) * 2019-06-26 2023-11-07 海南中和药业股份有限公司 一种固相片段法合成比伐卢定
CN115073587B (zh) * 2022-07-08 2024-08-23 厦门胜泽泰医药科技有限公司 一种半连续液相合成比伐芦定的合成工艺

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI904330A7 (fi) * 1988-09-29 1990-09-03 Biogen Inc Hirudiinipeptidejä
US5196404B1 (en) 1989-08-18 1996-09-10 Biogen Inc Inhibitors of thrombin
GB9708918D0 (en) 1997-05-01 1997-06-25 Ppl Therapeutics Scotland Ltd Methods
CN1688606A (zh) * 2002-08-12 2005-10-26 昆士兰医学研究所理事会 含有辅助t细胞和b细胞表位的新的免疫原性脂肽
CA2543930A1 (fr) * 2003-10-30 2005-05-12 The University Of Massachusetts Nouveaux agents de couplage destines a une synthese peptidique
JP4903709B2 (ja) * 2004-10-19 2012-03-28 ロンザ アーゲー 固相ペプチド合成のための方法
ZA200707006B (en) * 2005-01-25 2008-11-26 Cell Therapeutics Inc Conjugates of biologically active proteins having a modified in vivo half-life
KR101608083B1 (ko) 2005-01-25 2016-04-01 씨티아이 바이오파마 코포레이션 생체내 반감기가 변경된, 생물학적 활성을 갖는 단백질의접합체
MX2008003552A (es) * 2005-09-14 2008-11-12 Novetide Ltd Proceso para la produccion de bivalirudina.
US20070213505A1 (en) * 2006-03-08 2007-09-13 David Epstein Solution Synthesis of Peptide Cell Growth Stimulators
CN101033249B (zh) * 2006-03-10 2011-05-11 周逸明 固相多肽合成比筏芦定的制备方法
KR101634830B1 (ko) * 2008-09-03 2016-06-29 시노팜 타이완 리미티드 비발리루딘의 제조방법

Also Published As

Publication number Publication date
AU2009335350A1 (en) 2011-07-21
TW201500378A (zh) 2015-01-01
CN102264757B (zh) 2014-05-21
ES2439502T3 (es) 2014-01-23
EP2382232A1 (fr) 2011-11-02
EA201101015A1 (ru) 2012-02-28
JP2015107967A (ja) 2015-06-11
TWI599580B (zh) 2017-09-21
TW201024317A (en) 2010-07-01
MX2011006950A (es) 2011-07-28
US8921517B2 (en) 2014-12-30
WO2010075983A1 (fr) 2010-07-08
US20150080550A1 (en) 2015-03-19
CA2744627C (fr) 2016-08-16
IL213457A0 (en) 2011-07-31
CN103864894B (zh) 2019-08-23
JP5996618B2 (ja) 2016-09-21
CN103864894A (zh) 2014-06-18
KR101653950B1 (ko) 2016-09-05
ZA201104195B (en) 2012-04-25
IL213457A (en) 2016-06-30
DK2382232T3 (da) 2013-12-16
TW201630927A (zh) 2016-09-01
HK1162527A1 (zh) 2012-08-31
AR074944A1 (es) 2011-02-23
CA2916716C (fr) 2018-06-26
CN103864895A (zh) 2014-06-18
CA2916716A1 (fr) 2010-07-08
JP2012514015A (ja) 2012-06-21
TWI538919B (zh) 2016-06-21
TWI453216B (zh) 2014-09-21
CO6400148A2 (es) 2012-03-15
CN102264757A (zh) 2011-11-30
JP5730781B2 (ja) 2015-06-10
CA2744627A1 (fr) 2010-07-08
KR20110112385A (ko) 2011-10-12
US20110251372A1 (en) 2011-10-13
EP2382232B1 (fr) 2013-09-18
SG171859A1 (en) 2011-07-28

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